Elsevier

Metabolism

Volume 39, Issue 9, Supplement 2, September 1990, Pages 78-81
Metabolism

Distribution of somatostatin receptors in normal and tumor tissue

https://doi.org/10.1016/0026-0495(90)90217-ZGet rights and content

Abstract

Specific receptors for somatostatin (SS), mediating the various actions of this peptide, have been described in SS target tissues in animal and man. Using homogenate binding assays, as well as receptor autoradiography, the presence of SS receptors has been demonstrated in various regions of the brain (cortex, limbic system, basal ganglia), the anterior pituitary, the endocrine and exocrine pancreas, the gastrointestinal tract, and the adrenals. There are species-, as well as age-, related variations. Furthermore, there is evidence for different SS receptor subtypes. Interestingly, a large variety of human tumors also contain SS receptors with similar characteristics as those found in normal tissue; in numerous tumors, the SS receptor density is even higher than in healthy tissue counterparts. Most GH- and TSH-producing pituitary adenomas, but also a subgroup of endocrine inactive pituitary adenomas, have SS receptors; most carcinoids and islet cell carcinomas, as well as their metastases, also contain SS receptors. Several differentiated (usually EGF receptor negative) glia tumors possess SS receptors, whereas indifferentiated (EGF receptor positive) glia tumors lack such receptors. Furthermore, a subgroup of breast tumors, usually steroid receptor positive and neuroendocrine-differentiated, contain SS receptors. Finally, small cell lung carcinomas, but not non-small cell carcinomas, often possess SS receptors. These receptors are likely to be functional since in 11 acromegalics and 18 gastroenteropancreatic tumor patients, a positive correlation was observed between their SS receptor status and their hormone secretion sensitivity to Sandostatin®. The presence of SS receptors in several types of endocrine-related human tumors may, therefore, represent the molecular basis for the therapeutical efficacy of SS analogues. In addition, SS receptor bearing tumors and their metastases have recently been shown to be easily diagnosed and precisely localized in the patient after in vivo labeling of the tumoral SS receptors with 123I-Tyr3-Sandostatin. Therefore, knowledge of tumoral SS receptor status may be of great importance in order to facilitate therapeutical decisions in patients bearing endocrine-related tumors.

References (33)

  • JC Reubi

    Evidence of two somatostatin-14 receptor types in rat brain cortex

    Neurosci Lett

    (1984)
  • JE Taylor et al.

    In vitro and in vivo inhibition of human small cell lung carcinoma (NCI-H69) growth by a somatostatin analogue

    Biochem Biophys Res Commun

    (1988)
  • C Srikant et al.

    Receptor binding of somatostatin-28 is tissue specific

    Nature

    (1981)
  • A Enjalbert et al.

    Somatostatin receptors on rat anterior pituitary membranes

    Endocrinology

    (1982)
  • FJ Reyl et al.

    Intracellular receptor for somatostatin in gastric mucosal cells: Decomposition and reconstitution of somatostatin-stimulated phosphoprotein phosphatases

  • N Viguerie et al.

    Functional somatostatin receptors on a rat pancreatic acinar cell line

    Am J Physiol

    (1988)
  • Cited by (232)

    • Effects of adding an albumin binder chain on [<sup>177</sup>Lu]Lu-DOTATATE

      2018, Nuclear Medicine and Biology
      Citation Excerpt :

      177Lu]Lu-DOTA-EB-TATE was able to deliver 7.9 fold higher tumour dose compared to [177Lu]Lu-DOTATATE, but this was also accompanied with 3.2 and 18.2 fold dose increase for kidneys and bone marrow respectively. Interestingly, the addition of our albumin binders to [177Lu]Lu-DOTATATE, decreased pancreas, adrenal, and lung uptake significantly; those tissues are known to normally express SST receptors [24,25]. It is possible that the addition of an albumin binding moiety has altered the affinity profile for other SSTR receptors, thought this would require further investigation.

    • Chapter 65-Pancreatic neuroendocrine tumors: Classification, clinical picture, diagnosis, and therapy

      2016, Blumgart's Surgery of the Liver, Biliary Tract and Pancreas: Sixth Edition
    • Biochemical Diagnosis and Preoperative Imaging of Gastroenteropancreatic Neuroendocrine Tumors

      2016, Surgical Oncology Clinics of North America
      Citation Excerpt :

      These G-protein-coupled receptors are normally expressed by neuroendocrine cells in a wide variety of tissue types, including the brain, pituitary, pancreas, thyroid, spleen, adrenal glands, large and small intestine, kidney, peripheral nervous system, immune cells, and the vasculature.99–101 SSTR2 is the most highly expressed SSTR subtype on most well-differentiated NETs and is the primary receptor for somatostatin-based imaging and treatment.99,102 There are 2 types of somatostatin receptor-based imaging available.

    View all citing articles on Scopus
    View full text